Anatoly Mazurov,Lan Miao,Yunde Xiao,Philip S. Hammond,Craig H. Miller,Srinivasa Rao Akireddy,Srinivasa V. Murthy,Regina C. Whitaker,Scott R. Breining,Matt S. Melvin
申请号：
US14922473
公开号：
US09580434B2
申请日:
2015.10.26
申请国别(地区):
US
年份:
2017
代理人:
摘要：
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
